EP1942105A4 - Aminodihydrothiazine derivative - Google Patents

Aminodihydrothiazine derivative

Info

Publication number: EP1942105A4
Authority: EP; European Patent Office
Prior art keywords: aminodihydrothiazine derivative; aminodihydrothiazine; derivative
Prior art date: 2005-10-25
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Granted

Application number

EP06822035A

Other languages

German (de)

French (fr)

Other versions

EP1942105A1 (en

EP1942105B1 (en

EP1942105B8 (en

Inventor

Naotake Kobayashi

Kazuo Ueda

Naohiro Itoh

Shinji Suzuki

Gaku Sakaguchi

Akira Kato

Akira Yukimasa

Akihiro Hori

Yuji Koriyama

Hidekazu Haraguchi

Ken Yasui

Yasuhiko Kanda

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Shionogi and Co Ltd

Original Assignee

Shionogi and Co Ltd

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2005-10-25

Filing date

2006-10-23

Publication date

2011-06-15

2006-10-23 Application filed by Shionogi and Co Ltd filed Critical Shionogi and Co Ltd

2006-10-23 Priority to EP13150550.5A priority Critical patent/EP2597087B1/en

2006-10-23 Priority to EP20130150548 priority patent/EP2612854B1/en

2008-07-09 Publication of EP1942105A1 publication Critical patent/EP1942105A1/en

2011-06-15 Publication of EP1942105A4 publication Critical patent/EP1942105A4/en

2014-04-16 Publication of EP1942105B1 publication Critical patent/EP1942105B1/en

2014-08-13 Application granted granted Critical

2014-08-13 Publication of EP1942105B8 publication Critical patent/EP1942105B8/en

Status Not-in-force legal-status Critical Current

2026-10-23 Anticipated expiration legal-status Critical

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A—HUMAN NECESSITIES
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- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
- A—HUMAN NECESSITIES
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- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- C—CHEMISTRY; METALLURGY
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/12—Nitrogen atoms not forming part of a nitro radical
- C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
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- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/18—Nitrogen atoms
- C—CHEMISTRY; METALLURGY
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- C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Molecular Biology (AREA)
Biophysics (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Dermatology (AREA)
Psychology (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Ophthalmology & Optometry (AREA)
Vascular Medicine (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Thiazole And Isothizaole Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

EP20060822035 2005-10-25 2006-10-23 Aminodihydrothiazine derivative Not-in-force EP1942105B8 (en)

Priority Applications (2)

Application Number	Priority Date	Filing Date	Title
EP13150550.5A EP2597087B1 (en)	2005-10-25	2006-10-23	Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
EP20130150548 EP2612854B1 (en)	2005-10-25	2006-10-23	Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
JP2005309642		2005-10-25
JP2006076636		2006-03-20
PCT/JP2006/321015 WO2007049532A1 (en)	2005-10-25	2006-10-23	Aminodihydrothiazine derivative

Related Child Applications (4)

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EP20130150548 Division EP2612854B1 (en)	2005-10-25	2006-10-23	Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
EP20130150548 Division-Into EP2612854B1 (en)	2005-10-25	2006-10-23	Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
EP13150550.5A Division EP2597087B1 (en)	2005-10-25	2006-10-23	Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors
EP13150550.5A Division-Into EP2597087B1 (en)	2005-10-25	2006-10-23	Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors

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EP20060822035 Not-in-force EP1942105B8 (en)	2005-10-25	2006-10-23	Aminodihydrothiazine derivative
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EP13150550.5A Not-in-force EP2597087B1 (en)	2005-10-25	2006-10-23	Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors

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EP13150550.5A Not-in-force EP2597087B1 (en)	2005-10-25	2006-10-23	Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors

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KR (1)	KR101052122B1 (en)
CN (2)	CN103936690B (en)
AU (1)	AU2006307314C1 (en)
BR (1)	BRPI0617852A2 (en)
CA (1)	CA2628074C (en)
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US20130158260A1 (en)	2013-06-20
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EP2612854B1 (en)	2015-04-29
EP1942105A1 (en)	2008-07-09
US9029358B2 (en)	2015-05-12
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AU2006307314C1 (en)	2011-08-25
RU2416603C9 (en)	2012-06-20
US8546380B2 (en)	2013-10-01
CN103936690A (en)	2014-07-23
EP2612854A1 (en)	2013-07-10
US20090082560A1 (en)	2009-03-26
US8173642B2 (en)	2012-05-08
CN101346357A (en)	2009-01-14
WO2007049532A1 (en)	2007-05-03
US8633188B2 (en)	2014-01-21
CN101346357B (en)	2014-04-02
CA2628074A1 (en)	2007-05-03
KR101052122B1 (en)	2011-07-26
JPWO2007049532A1 (en)	2009-04-30
BRPI0617852A2 (en)	2011-08-09
RU2010151410A (en)	2012-06-20
ES2537898T3 (en)	2015-06-15
ES2572263T3 (en)	2016-05-31
EP2597087B1 (en)	2016-03-30
CN103936690B (en)	2016-06-08
EP1942105B1 (en)	2014-04-16
US20120022249A1 (en)	2012-01-26
ES2476027T3 (en)	2014-07-11
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CA2628074C (en)	2014-01-14
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EP2597087A1 (en)	2013-05-29
US20150210680A1 (en)	2015-07-30
US8815851B2 (en)	2014-08-26
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JP5281794B2 (en)	2013-09-04
JP5608250B2 (en)	2014-10-15
TWI451869B (en)	2014-09-11
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ZA200711025B (en)	2008-12-31	N-dihydroxyalkyl-substituted 2-oxoimidazole derivative
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DE502006004337D1 (en)	2009-09-03	Strangführungsrolle
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GB0504960D0 (en)	2005-04-20	Benzoxazocines
ZA200708531B (en)	2009-02-25	Pyridylmethylsulfone derivative
IL184481A0 (en)	2007-10-31	Fluoroalkylpyrrolidine derivative

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